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    Method of producing polymeric phenazonium compounds
    52.
    发明授权
    Method of producing polymeric phenazonium compounds 有权
    生产聚合物苯扎嗪化合物的方法

    公开(公告)号：US08691987B2

    公开(公告)日：2014-04-08

    申请号：US12890013

    申请日：2010-09-24

    申请人： Andrew M. Krol ,  Ernest Long ,  Lev Taytsas

    发明人： Andrew M. Krol ,  Ernest Long ,  Lev Taytsas

    IPC分类号： C07D241/46

    CPC分类号： C08G73/0633 ,  C07D241/46 ,  C08G73/0694 ,  C25D3/38

    摘要： A process of making a polymeric phenazonium compound having the general formula: wherein R1, R2, R4, R5, R6, R8 and R9 are the same or different, and represent hydrogen, a low alkyl or a substituted aryl, R3 starts with NH2 and is diazotized followed by polymerization, R5 and R8 may alternatively represent monomeric or polymeric phenazonium radicals, R7 with its substituent group is a substituted amine, with RX and RY representing any combination of CH3, C2H5, and hydrogen, except that RX and RY cannot both be hydrogen, A is an acid radical, and n is an integer from 2 to 100, preferably from 2 to 20 is described. The polymeric phenazonium compound is usable in as an additive in a metal plating bath. The method includes the steps of: a) dissolving an effective amount of an amino compound in a formic acid solution; b) adding a nitrite salt to diazotize the amino compound; and c) adding sulfamic acid to neutralize any excess nitrous acid that may be formed in step b), whereby a polymeric phenazonium compound is produced.

    摘要翻译： 制备具有以下通式的聚合物苯扎嗪化合物的方法：其中R 1，R 2，R 4，R 5，R 6，R 8和R 9相同或不同，并且表示氢，低级烷基或取代的芳基，R 3从NH 2开始， 被重氮化，随后聚合，R 5和R 8可以代表单体或聚合物苯扎嗪基团，其取代基的R7是取代的胺，其中RX和RY表示CH 3，C 2 H 5和氢的任何组合，不同之处在于RX和RY不能同时 为氢，A为酸基，n为2〜100，优选为2〜20的整数。 聚合物苯扎嗪化合物可用作金属电镀浴中的添加剂。 该方法包括以下步骤：a）将有效量的氨基化合物溶于甲酸溶液中; b）加入亚硝酸盐以重氮化氨基化合物; 和c）加入氨基磺酸以中和步骤b）中可能形成的任何过量的亚硝酸，由此产生聚合的苯扎嗪化合物。

    Oral Formulations for Tetrapyrrole Derivatives
    55.
    发明申请
    Oral Formulations for Tetrapyrrole Derivatives 有权
    四吡咯衍生物的口服制剂

    公开(公告)号：US20100273803A1

    公开(公告)日：2010-10-28

    申请号：US12768244

    申请日：2010-04-27

    申请人： Susanna Gräfe ,  Nikolay Nifantiev ,  Albrecht Volker ,  Wolfgang Neuberger ,  Gerhard Wieland ,  Dietrich Scheglmann ,  Alfred Fahr ,  Arno Wiehe

    发明人： Susanna Gräfe ,  Nikolay Nifantiev ,  Albrecht Volker ,  Wolfgang Neuberger ,  Gerhard Wieland ,  Dietrich Scheglmann ,  Alfred Fahr ,  Arno Wiehe

    IPC分类号： A61K31/498 ,  C07D241/46 ,  A61K31/409 ,  C07D487/22 ,  A61P35/00 ,  A61P31/00 ,  A61K8/49 ,  A61Q19/00 ,  A61Q9/00

    CPC分类号： A61K31/409 ,  A61K9/0065 ,  A61K9/127 ,  A61K9/1271 ,  A61K31/498

    摘要： Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract.

    摘要翻译： 提出了在光动力治疗（PDT）和抗微生物光动力疗法（APDT）治疗中配制口服光敏剂的口服制剂和方法。 口服配制的光敏剂显示增加的溶解度和渗透性，从而提高光敏剂在治疗部位的生物利用度。 口服给药的光敏剂适于配制用于通过胃肠粘膜进行粘膜粘附和吸收。 本文提供的口服制剂通过口服途径使用脂质和已知蛋白质作为光敏剂的载体。 用于封装预选光敏剂的载体包括常规脂质体，聚乙二醇化脂质体，纳米乳剂，纳米胶体，纳米颗粒，脂肪乳剂，脂质制剂，水溶胶，SMEDDS，α-铁蛋白（AFP）和牛血清白蛋白（BSA），脂肪乳剂，热 熔融挤出物和纳米颗粒。 在本发明的疏水性光敏剂的情况下，使用合适的表面活性剂/增溶剂稳定口服制剂，从而防止药物在胃中的聚集，直到其被吸收到十二指肠和小肠中。 口服制剂可以以液体，胶囊，片剂，粉末，糊剂或凝胶的形式施用。 配制药物可以在给予PDT之前以一次剂量或多次剂量口服给药。 在一个实施方案中，Temoporfin（m-THPC）用作口服制剂中的光敏剂。 类似于许多疏水性光敏剂的Temoporfin特别适合于口服给药，因为哺乳动物体内没有已知的可以代谢Temoporfin或类似光敏剂的酶系统。 Temoporfin可以在胃肠道吸收制剂后达到血液系统不变和充分活性。

    Phenylaminopropanol Derivatives and Methods of Their Use
    56.
    发明申请
    Phenylaminopropanol Derivatives and Methods of Their Use 失效
    苯胺基丙醇衍生物及其使用方法

    公开(公告)号：US20080255102A1

    公开(公告)日：2008-10-16

    申请号：US12144363

    申请日：2008-06-23

    申请人： An Thien Vu ,  Paige Erin Mahaney ,  Stephen Todd Cohn

    发明人： An Thien Vu ,  Paige Erin Mahaney ,  Stephen Todd Cohn

    IPC分类号： A61K31/538 ,  C07D403/06 ,  C07D265/36 ,  C07D209/04 ,  A61K31/404 ,  A61K31/5415 ,  A61P25/00 ,  A61P15/00 ,  A61K31/498 ,  C07D241/46 ,  C07D279/16 ,  A61K31/496

    CPC分类号： C07D279/16 ,  C07D209/08 ,  C07D241/42 ,  C07D265/36

    摘要： The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

    摘要翻译： 本发明涉及式I的苯基氨基丙醇衍生物：或其药学上可接受的盐，含有这些衍生物的组合物及其用于预防和治疗由单胺再摄取改善的病症的方法，所述方法尤其包括血管舒缩症状（VMS） 特别是选自重症抑郁障碍，血管舒缩症状，压力和急迫性尿失禁，纤维肌痛，疼痛等的那些病症，其中，所述疾病，性功能障碍，胃肠道和泌尿生殖系统疾病，慢性疲劳综合征，纤维肌痛综合征，神经系统疾病及其组合， 糖尿病性神经病变及其组合。

    Novel one-dimensional coordination polymer
    58.
    发明申请
    Novel one-dimensional coordination polymer 审中-公开
    新型一维配位聚合物

    公开(公告)号：US20050203273A1

    公开(公告)日：2005-09-15

    申请号：US11074763

    申请日：2005-03-09

    申请人： Masato Kitamura ,  Keiji Nakano

    发明人： Masato Kitamura ,  Keiji Nakano

    IPC分类号： C07D241/38 ,  C07D241/46 ,  C07F1/08 ,  C07F15/04 ,  C08G79/00 ,  C08G61/00

    CPC分类号： C08G79/00

    摘要： A one-dimensional coordination polymer having a linear structure and represented by general formula (I) given below: where M denotes copper or nickel, X denotes a halogen atom, R denotes a pyrazine derivative represented by general formula (II) given below, and n is an integer: where each of Z1 and Z2, which may be the same or different, denotes an atomic group required for forming a carbon ring by joining with a methylene chain the carbon atoms in the 2-position and 3-position or the carbon atoms in the 5-position and 6-position of the pyrazine ring, and * denotes the binding position with M included in general formula (I).

    摘要翻译： 具有线性结构并由下式给出的通式（I）表示的一维配位聚合物：其中M表示铜或镍，X表示卤素原子，R表示下述通式（II）表示的吡嗪衍生物，和 n是整数，其中Z 1和Z 2各自可以相同或不同，表示通过与一个或多个碳原子连接形成碳环所需的原子团 亚甲基链是吡嗪环的2-位和3-位的碳原子或5-位和6-位的碳原子，*表示与通式（I）中包含的M的结合位置。

    Process for manufacture of in vivo stain composition
    59.
    发明申请
    Process for manufacture of in vivo stain composition 有权
    制造体内染色组合物的方法

    公开(公告)号：US20010007904A1

    公开(公告)日：2001-07-12

    申请号：US09759808

    申请日：2001-01-11

    发明人： Douglas D. Burkett

    IPC分类号： C07D241/46

    CPC分类号： A61K49/006 ,  C07D279/20 ,  C09B21/00 ,  G01N30/34 ,  G01N30/36 ,  G01N2030/027

    摘要： A process for synthesizing 2-amino-5-dimethlyaminophenyl thiosulfonic acid comprises the step of oxidizing N,Nnull-dimethyl-null-phenylene-diamine in the presence of a source of thiosulfate ions, while maintaining the temperature of the reaction mixture not higher than about 10null C. This compound is useful as an intermediate in the synthesis of toluidine blue O. A process for manufacturing toluidine blue O with improved yield, includes the step of preparing the intermediate 2-amino-5-diethylaminopropyl thiosulfonic acid according to the above described procedure.

    摘要翻译： 合成2-氨基-5-二甲氨基苯基硫代磺酸的方法包括在硫代硫酸根离子源存在下氧化N，N'-二甲基 - 对 - 苯二胺的步骤，同时保持反应混合物的温度不高 该化合物可用作甲苯胺蓝O的合成中的中间体。具有提高的产率的制备甲苯胺蓝O的方法包括根据以下步骤制备中间体2-氨基-5-二乙基氨基丙基硫代磺酸的步骤： 上述步骤。

    Electrochromic compounds
    60.
    发明授权
    Electrochromic compounds 有权
    电致变色化合物

    公开(公告)号：US6037471A

    公开(公告)日：2000-03-14

    申请号：US140310

    申请日：1998-08-26

    申请人： Ramanujan Srinivasa ,  Darla J. French ,  Rongguang Lin ,  Thomas F. Guarr ,  Harlan J. Byker ,  Kelvin L. Baumann ,  David A. Theiste

    发明人： Ramanujan Srinivasa ,  Darla J. French ,  Rongguang Lin ,  Thomas F. Guarr ,  Harlan J. Byker ,  Kelvin L. Baumann ,  David A. Theiste

    IPC分类号： C07D213/22 ,  C07D241/36 ,  C07D241/46 ,  C09K9/02 ,  G02F1/15

    CPC分类号： C07D213/22 ,  C07D241/36 ,  C07D241/46 ,  C09K9/02 ,  G02F1/1521

    摘要： An improved electrochromic device, the device incorporating an electrochromic medium that comprises at least three electroactive materials having absorption spectra that add together such that the color of the electrochromic medium can be pre-selected by individually choosing the concentrations of the at least three electroactive materials. The electrochromic medium generally maintains the pre-selected perceived color throughout its normal range of voltages when used in an electrochromic device. The at least three electroactive materials include at least one electrochemically reducible material (cathodic material), at least one electrochemically oxidizable material (anodic material) and at least one additional electroactive material which may be either an anodic or cathodic material. Thus, there are always three electroactive materials present in the medium, with at least two either being anodic or cathodic materials. The pre-selected color may be chosen from a wide variety of colors and may be, for example, red, orange, yellow, green, blue, purple. For electrochromic mirrors for motor vehicles, a presently preferred color is gray.

    摘要翻译： 一种改进的电致变色装置，该装置包含电致变色介质，其包含至少三种具有吸收光谱的电活性材料，所述电活性材料相加在一起，使得电致变色介质的颜色可以通过单独选择至少三种电活性材料的浓度来预先选择。 当电致变色装置中使用时，电致变色介质通常保持其预定的感知颜色在其正常的电压范围内。 至少三种电活性材料包括至少一种电化学可还原材料（阴极材料），至少一种电化学可氧化材料（阳极材料）和至少一种额外的电活性材料，其可以是阳极或阴极材料。 因此，介质中总是存在三种电活性材料，至少有两种是阳极或阴极材料。 预选颜色可以从各种颜色中选择，并且可以是例如红，橙，黄，绿，蓝，紫。 对于用于机动车辆的电致变色镜，目前优选的颜色是灰色。